Document Type
Article
Publication Date
5-1-2018
College/Unit
School of Pharmacy
Department/Program/Center
Pharmaceutical Sciences
Abstract
Sixteen disulfides derived from disulfiram (Antabuse™) were evaluated as antibacterial agents. Derivatives with hydrocarbon chains of seven and eight carbons in length exhibited antibacterial activity against Gram-positive Staphylococcus, Streptococcus, Enterococcus, Bacillus, and Listeria spp. A comparison of the cytotoxicity and microsomal stability with disulfiram further revealed that the eight carbon chain analog was of lower toxicity to human hepatocytes and has a longer metabolic half-life. In the final analysis, this investigation concluded that the S-octylthio derivative is a more effective growth inhibitor of Gram-positive bacteria than disulfiram and exhibits more favorable cytotoxic and metabolic parameters over disulfiram.
Digital Commons Citation
Sheppard, Jordan G.; Frazier, Keely R.; Saralkar, Pushkar; Hossain, Mohammad F.; Geldenhuys, Werner J.; and Long, Timothy E., "Disulfiram-based disulfides as narrow-spectrum antibacterial agents" (2018). Clinical and Translational Science Institute. 804.
https://researchrepository.wvu.edu/ctsi/804
Source Citation
Sheppard JG, Frazier KR, Saralkar P, Hossain MF, Geldenhuys WJ, Long TE. Disulfiram-based disulfides as narrow-spectrum antibacterial agents. Bioorganic & Medicinal Chemistry Letters. 2018;28(8):1298-1302. doi:10.1016/j.bmcl.2018.03.023
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